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1. 发明授权

US5053526A Pharmaceuticals containing prostaglandin I.sub.2 失效
标题翻译：含有前列腺素I2的药物
公开(公告)号：US5053526A
公开(公告)日：1991-10-01
申请号：US511945
申请日：1990-04-16
申请人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa , Toshiaki Mase , Akira Ishibashi , Daijiro Horii , Toshiji Kanayama , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Ishiyama , Yoshio Hayashi
发明人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa , Toshiaki Mase , Akira Ishibashi , Daijiro Horii , Toshiji Kanayama , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Ishiyama , Yoshio Hayashi
IPC分类号： A61K31/557 , C07C405/00
CPC分类号： C07C405/0083 , A61K31/557
摘要： Disclosed is a pharmaceutical having circulation ameliorating effect and antiulcer effect containing a prostaglandin I.sub.2 analogue represented by the formula shown below or a non-toxic salt of its salt or a cyclodextrin inclusion compound thereof as the effective ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms or a phenyl group; A represents a pentyl group, a cyclopentyl group, a cyclohexyl group, a 1-methyl-3-hexynyl group, a 2-methyl-3-hexynyl group, a 1-methylhexyl group, a 2-phenethyl group, a 1,1-dimethylpentyl group, a 2-methylpentyl group, a 1-cyclohexylethyl group, a 2-methylhexyl group, a 1-methyl-3-pentynyl group or 1 2,6-dimethyl-5-heptenyl group; the double bond between the carbon atoms at 4- and 5-positions is E or Z or a mixture thereof, the asymmetric center in the substituent represented by A is R-configuration or S-configuration or a mixture thereof.The pharmaceuticals containing, as an active ingredient, prostaglandin I.sub.2 analogues of the present invention have potent platelet aggregation inhibiting effect, blood pressure depressing effect, vasodilative effect and antiulcer effect, and are also low in toxicity.
摘要翻译：本发明公开了一种具有循环改善作用和抗溃疡效果的药物，其含有下述式表示的前列腺素I2类似物或其盐的无毒性盐或其环糊精包合物作为有效成分：其中R1表示氢原子，碳原子数1〜12的烷基，碳原子数4〜7的环烷基或苯基; A表示戊基，环戊基，环己基，1-甲基-3-己炔基，2-甲基-3-己炔基，1-甲基己基，2-苯乙基，1,1 2-甲基戊基，2-甲基戊基，1-环己基乙基，2-甲基己基，1-甲基-3-戊炔基或1,6-二甲基-5-庚烯基; 在4-和5-位碳原子之间的双键是E或Z或其混合物，由A表示的取代基中的不对称中心是R-构型或S-构型或其混合物。含有本发明的前列腺素I2类似物作为活性成分的药物具有有效的血小板聚集抑制作用，降血压作用，血管扩张作用和抗溃疡作用，毒性也低。

2. 发明授权

US4699921A Pharmaceuticals containing prostaglandin I.sub.2 失效
标题翻译：含有前列腺素I2的药物
公开(公告)号：US4699921A
公开(公告)日：1987-10-13
申请号：US763618
申请日：1985-08-08
申请人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa , Toshiaki Mase , Akira Ishibashi , Daijiro Horii , Toshiji Kanayama , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Ishiyama , Yoshio Hayashi
发明人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa , Toshiaki Mase , Akira Ishibashi , Daijiro Horii , Toshiji Kanayama , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Ishiyama , Yoshio Hayashi
IPC分类号： C07C59/46 , A61K31/557 , A61P1/04 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/12 , C07C51/00 , C07C67/00 , C07C69/732 , C07C405/00
CPC分类号： C07C405/0083 , A61K31/557 , Y02P20/55
摘要： Disclosed is a pharmaceutical composition having circulation ameliorating effect and antiulcer effect containing a prostaglandin I.sub.2 analogue represented by the formula shown below or a non-toxic salt or a cyclodextrin inclusion compound thereof as the effective ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms or a phenyl group, A represents a pentyl group, a cyclopentyl group, a cyclohexyl group, a 1-methyl-3-hexynyl group, a 2-methyl-3-hexynyl group, a 1-methylhexyl group, a 2-phenethyl group, a 1,1-dimethylpentyl group, a 2-methylpentyl group, a 1-cyclohexylethyl group, a 2-methylhexyl group, a 1-methyl-3-pentynyl group or a 2,6-dimethyl-5-heptenyl group; the double bond between the carbon atoms at 4- and 5-positions is E or Z or a mixture thereof; the asymmetric center in the substituent represented by A is in the R-configuration or the S-configuration or a mixture thereof.Pharmaceutical compositions containing, as an active ingredient, prostaglandin I.sub.2 analogues of the present invention have potent platelet aggregation inhibiting effect, blood pressure depressing effect, vasodilative effect and antiulcer effect, and are also low in toxicity.
摘要翻译：本发明公开了一种具有循环改善作用和抗溃疡效果的药物组合物，其含有下述式表示的前列腺素I 2类似物或其无毒性盐或环糊精包合物作为有效成分：其中R 1表示氢原子，碳原子数1〜12的烷基，碳原子数4〜7的环烷基或苯基，A表示戊基，环戊基，环己基，1-甲基-3-己炔基，2 1-甲基-3-己炔基，1-甲基己基，2-苯乙基，1,1-二甲基戊基，2-甲基戊基，1-环己基乙基，2-甲基己基，1-甲基 -3-戊炔基或2,6-二甲基-5-庚烯基; 4-和5-位的碳原子之间的双键是E或Z或它们的混合物; 由A表示的取代基中的不对称中心是R构型或S-构型或其混合物。含有本发明的前列腺素I2类似物作为活性成分的药物组合物具有有效的血小板聚集抑制作用，降血压作用，血管扩张作用和抗溃疡作用，毒性也低。

3. 发明授权

US4681951A Bicyclo(3.3.0)octene derivatives 失效
标题翻译：双环（3.3.0）辛烯衍生物
公开(公告)号：US4681951A
公开(公告)日：1987-07-21
申请号：US641587
申请日：1984-08-17
申请人： Masakatsu Shibasaki , Toshiaki Mase , Mikiko Sodeoka , Yuji Ogawa
发明人： Masakatsu Shibasaki , Toshiaki Mase , Mikiko Sodeoka , Yuji Ogawa
IPC分类号： C07C405/00 , C07F7/18 , C07D309/10 , C07C47/40
CPC分类号： C07F7/1856 , C07C405/0016 , C07C405/0025 , C07C405/0083 , Y02P20/55
摘要： There are disclosed bicyclo[3.3.0]octene derivatives having the following formula: ##STR1## wherein R.sup.1 is a straight, branched or cyclic alkyl group or alkenyl group each having 5 to 10 carbon atoms; andR.sup.2 and R.sup.3 are each separately a hydrogen atom or a protective group of a hydroxy group,and process for producing the same. These compounds and the process for producing them are available for producing a 9(0)-methano-.DELTA.6(9.alpha.)-PGI.sub.1.
摘要翻译：公开了具有下式的双环[3.3.0]辛烯衍生物：其中R 1是各自具有5至10个碳原子的直链，支链或环状烷基或烯基; R2和R3各自独立地为氢原子或羟基的保护基，以及其制备方法。这些化合物及其制备方法可用于制备9（0） - 甲 - △DELTA 6（9α）-PGI1。

4. 发明授权

US4762936A Bicyclo(3.3.0)Octene derivatives 失效
标题翻译：双环（3.3.0）辛烯衍生物
公开(公告)号：US4762936A
公开(公告)日：1988-08-09
申请号：US940349
申请日：1986-12-11
申请人： Masakatsu Shibasaki , Toshiaki Mase , Mikiko Sodeoka , Yuji Ogawa
发明人： Masakatsu Shibasaki , Toshiaki Mase , Mikiko Sodeoka , Yuji Ogawa
IPC分类号： C07C405/00 , C07F7/18 , C07D309/10 , C07C47/40 , C07C35/26
CPC分类号： C07F7/1856 , C07C405/0016 , C07C405/0025 , C07C405/0083 , Y02P20/55
摘要： There are disclosed a bicyclo[3.3.0]octene derivatives having the following formula: ##STR1## wherein R.sup.1 : a straight, branched or cyclic alkyl group or alkenyl group each having 5 to 10 carbon atoms;R.sup.2 and R.sup.3 : each represent a hydrogen atom or a protective group of a hydroxy group; andR.sup.4 : --CH.dbd.CH--(CH.sub.2).sub.2 --COOR.sup.5 or --CH.sub.2 R.sup.6 ; whereR.sup.5 : a hydrogen atom or an alkyl group; andR.sup.6 : a hydroxy group, an acetyloxy group or a butenyl group,and process for producing the same. These compounds and the process for producing them are available for producing a 9(0)-methano-.DELTA..sup.6 (9.alpha.)-PGI.sub.1.
摘要翻译：公开了具有下式的双环[3.3.0]辛烯衍生物：其中R 1：各自具有5-10个碳原子的直链，支链或环状烷基或烯基; R2和R3各自表示氢原子或羟基的保护基; 和R 4：-CH = CH-（CH 2）2 -COOR 5或-CH 2 R 6; 其中R5为氢原子或烷基; 和R6：羟基，乙酰氧基或丁烯基，及其制备方法。这些化合物及其制备方法可用于制备9（0） - 甲 - △DELTA 6（9α）-PGI1。

5. 发明授权

US4777271A Isocarbacyclin derivatives and process for production thereof 失效
标题翻译：异卡环素衍生物及其制备方法
公开(公告)号：US4777271A
公开(公告)日：1988-10-11
申请号：US65218
申请日：1987-05-29
申请人： Masakatsu Shibasaki , Mikiko Sodeoka , Toshiaki Mase
发明人： Masakatsu Shibasaki , Mikiko Sodeoka , Toshiaki Mase
IPC分类号： C07D319/00 , C07C405/00 , C07D493/08 , C07D319/04
CPC分类号： C07C405/0083 , Y02P20/55
摘要： An isocarbacyclin derivative represented by the general formula ##STR1## wherein R.sup.1 represents a linear, branched or cyclic alkyl, alkenyl or alkynyl group having 5 to 10 carbon atoms, and R.sup.2 and R.sup.3 represent a hydrogen atom or a protective group for the hydroxyl group; and a process for production thereof.

6. 发明申请

US20090131664A1 Method for Producing 4(3H)-Quinazolinone Derivative 审中-公开
标题翻译：生产4（3H） - 喹唑啉酮衍生物的方法
公开(公告)号：US20090131664A1
公开(公告)日：2009-05-21
申请号：US11922479
申请日：2006-07-04
申请人： Atsushi Akao , Takehiko Iida , Takahiro Itoh , Toshiaki Mase , Kimihiko Sato , Naotaka Sawada , Chie Kadowaki , Takayuki Tsuritani , Nobuyoshi Yasuda
发明人： Atsushi Akao , Takehiko Iida , Takahiro Itoh , Toshiaki Mase , Kimihiko Sato , Naotaka Sawada , Chie Kadowaki , Takayuki Tsuritani , Nobuyoshi Yasuda
IPC分类号： C07D401/02
CPC分类号： C07D239/74
摘要： This invention is related to a method for producing 3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone comprising a step for reacting 2-methyl-5-trifluoromethyl-4H-3,1-benzoxazin-4-one with 4-[3-(1-pyrrolidinyl)propoxy]aniline or an acid-addition salt thereof, or 4-(1-cyclobutyl-4-piperidinoy9oxyaniline or acid addition salt thereof in the presence of an acid catalyst.
摘要翻译：本发明涉及一种制备3- {4- [3-（1-吡咯烷基）丙氧基]苯基} -5-三氟甲基-4（3H） - 喹唑啉酮的方法，该方法包括使2-甲基-5-三氟甲基 - 4H-3,1-苯并恶嗪-4-酮与4- [3-（1-吡咯烷基）丙氧基]苯胺或其酸加成盐或4-（1-环丁基-4-哌啶基）苯氧基苯胺或其酸加成盐在酸催化剂的存在。

7. 发明授权

US07439535B2 Process for exchanging functional groups by halogen-metal exchange reaction 失效
标题翻译：通过卤素 - 金属交换反应交换官能团的方法
公开(公告)号：US07439535B2
公开(公告)日：2008-10-21
申请号：US11077292
申请日：2005-03-11
申请人： Takehiko Iida , Toshihiro Wada , Toshiaki Mase
发明人： Takehiko Iida , Toshihiro Wada , Toshiaki Mase
IPC分类号： C07F3/02
CPC分类号： C07D213/84 , C07C45/004 , C07C45/45 , C07D213/61 , C07D333/28 , C07F3/02 , C07F7/0827 , C07C47/55
摘要： A method by which a halogen atom of a halogen compound can be efficiently replaced with an electrophilic group.Also provided are: a reagent for converting a functional group through a halogen-metal exchange reaction, characterized by comprising either a mixture of a magnesium compound represented by the formula R1—Mg—X (I) (wherein R1 represents a halogen atom or an optionally substituted hydrocarbon residue; and X1 represents a halogen atom) and an organolithium compound represented by the formula R2—Li (II)(wherein R2 represents an optionally substituted hydrocarbon residue) or a product of the reaction of the magnesium compound with the organolithium compound; and a process for producing with the reagent a compound in which a halogen atom of a halogen compound has been replaced with an electrophilic group.
摘要翻译：可以用亲电子基团有效地代替卤素化合物的卤素原子的方法。还提供：用于通过卤素 - 金属交换反应转化官能团的试剂，其特征在于包含由式R 1 -Mg-X（I）表示的镁化合物的混合物（其中R 1表示卤素原子或任选取代的烃残基; X 1表示卤素原子）和由式R 2表示的有机锂化合物，（II）（其中R 2表示任选取代的烃残基）或镁化合物与有机锂化合物的反应的产物; 以及用该试剂制备其中卤素化合物的卤素原子已被亲电子基团取代的化合物的方法。

8. 发明申请

US20050176968A1 Process for producing indolopyrrolocarbazole derivative 审中-公开
标题翻译：吲哚吡咯并咔唑衍生物的制备方法
公开(公告)号：US20050176968A1
公开(公告)日：2005-08-11
申请号：US10524274
申请日：2003-08-22
申请人： Atsushi Akao , Masashi Kawasaki , Asayuki Kamatani , Toshiaki Mase
发明人： Atsushi Akao , Masashi Kawasaki , Asayuki Kamatani , Toshiaki Mase
IPC分类号： B01J23/46 , C07D487/14 , C07H19/23
CPC分类号： B01J31/0247 , B01J21/04 , B01J21/18 , B01J23/464 , B01J27/053 , B01J27/232 , B01J31/0244 , B01J31/04 , B01J31/2234 , B01J31/28 , B01J31/30 , B01J2231/641 , B01J2531/84 , C07D487/14 , C07H19/23
摘要： The present invention provides a process for industrially advantageously producing a compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, which is useful as an anticancer agent, and also provides a catalyst used for hydrogenation reaction in the process.
摘要翻译：本发明提供了一种工业上有利地制备式（I）表示的化合物或其药学上可接受的盐的方法，其可用作抗癌剂，并且还提供了用于该方法中的氢化反应的催化剂。

9. 发明授权

US5444152A Endothelin antagonistic peptide derivatives 失效
标题翻译：内皮素拮抗肽衍生物
公开(公告)号：US5444152A
公开(公告)日：1995-08-22
申请号：US214679
申请日：1994-03-21
申请人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano
发明人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/083 , C07K5/103 , A61K38/06
CPC分类号： C07K5/06156 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/0808 , C07K5/1008 , A61K38/00
摘要： Peptides having the formula ##STR1## inhibit the binding of endothelin to its receptor and are useful in treating diseases associated with excess production or secretion of endothelin.
摘要翻译：具有式“IMAGE”（I）的肽抑制内皮素与其受体的结合，并且可用于治疗与过量产生或分泌内皮素相关的疾病。

10. 发明授权

US07482449B2 Process for making spirolactone compounds 失效
标题翻译：制备螺内酯化合物的方法
公开(公告)号：US07482449B2
公开(公告)日：2009-01-27
申请号：US12077419
申请日：2008-03-19
申请人： Ralph P. Volante , David M. Tschaen , Steven A. Weissman , Matthew Heileman , Toshiaki Mase , Takehiko Iida , Kenji Maeda , Toshihiro Wada , Hiroki Sato , Kenichi Asakawa
发明人： Ralph P. Volante , David M. Tschaen , Steven A. Weissman , Matthew Heileman , Toshiaki Mase , Takehiko Iida , Kenji Maeda , Toshihiro Wada , Hiroki Sato , Kenichi Asakawa
IPC分类号： C07D405/12 , C07D405/14 , C07D307/94 , C07D491/107
CPC分类号： C07D493/10
摘要： This invention relates to a process for making spirolactone compounds analogous to formula I.
摘要翻译：本发明涉及类似于式I的制备螺内酯化合物的方法。

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